JNJ-64264681 | BTK inhibitor | Probechem Biochemicals

Chemical Structure : JNJ-64264681

JNJ-64264681 (JNJ 64264681)

Catalog No.: PC-49425Not For Human Use, Lab Use Only.

JNJ-64264681 is a potent, selective, covalent, irreversible BTK inhibitor with Ki of 48.5 nM, enzymatic IC50 of 558 nM.

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Biological Activity

JNJ-64264681 is a potent, selective, covalent, irreversible BTK inhibitor with Ki of 48.5 nM, enzymatic IC50 of 558 nM.

has IC50 of 99 nM in mouse CD69 splenocyte assay triggering B-cell activation by anti-IgM stimulation.

JNJ-64264681 targets BTK Cys481 with IC50 of 21 nM in enzyme-linked immunosorbent assay.

JNJ-64264681 shows antiproliferative activity (IC50<100 nM) against a panel of ABC-DLBCL cell lines─OCI-Ly3, OCI-Ly10, TMD8, and HBL-1, and CD79b mutant ABC-DLBCL cell lines (OCI-Ly10, TMD8, and HBL-1).

JNJ-64264681 (10, 30, and 100 mg/kg administered QD) inhibited tumor growth by 24%, 35%, and 51% TGI (30, 45, and 65% ΔTGI), respectively, in OCI-Ly10 human DLBCL xenografts in NSG mice.

Physicochemical Properties

M.Wt	518.636
Formula	C27H30N6O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-((1R,2S)-2-acrylamidocyclopentyl)-5-(6-isobutyl-4-methylpyridin-3-yl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide

References

1. Tichenor MS, et al. J Med Chem. 2022 Nov 10;65(21):14326-14336.

JNJ-64264681 (JNJ 64264681)

Biological Activity

Physicochemical Properties

References

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